(+)-Aphidicolin (Synonyms: ICI 69653, NSC 234714) |
| Catalog No.GC10867 |
Aphidicolina ((+)-Aphidicolina), un inhibidor reversible de la replicación del ADN nuclear eucariota, puede bloquear el ciclo celular en la fase pre-S[1].
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 38966-21-1
Sample solution is provided at 25 µL, 10mM.
Aphidicolin ((+)-Aphidicolin), a reversible inhibitor of eukaryotic nuclear DNA replication, can block the cell cycle at the pre-S phase[1]. The minimal concentration of aphidicolin required to produce reversible inhibition of DNA replication without toxic effects in embryos to be 0.5 µM[2].
In vitro experiment it shown that treatment with APC (Aphidicolin) at 6 μM in PBMC cell did not impact baseline DNA damage but could reliably block DNA repair after H2O2 challenge in both fresh and cryopreserved samples[3]. In vitro, treatment with 20 μM aphidicolin for 24 h in bovine aortic ECs (BAECs) reduced BAEC viability by ~40%, which was accompanied by increased NO production, phosphorylation of eNOS at Ser1179 (p-eNOS-Ser1179 were not altered by 1,2-bis (2-aminophenoxy)ethane-N,N,N',N'-tetraacetic acid tetrakis(acetoxymethyl ester) (BAPTA-AM), a cell permeable and specific intracellular Ca2+ chelator[4]. In addition, 5 x 10(-7) M aphidicolin can kill all cells of four human neuroblastoma cell lines as an agent which selectively kills neuroblastoma cells in vitro [5].
In vivo efficacy test it indicated that 4.5 mg aphidicolin/kg body weight was the maximum aphidicolin dose that could be applied as liposomal preparation that tested in neuroblastoma-bearing (UKF-NB-3) mice[6]. Aphidicolin glycinate (has higher solubility agent) (100 mg/kg; i.p.; once every 3 hfor 9 days) showed anti-tumor activity against the implanted B16 melanoma and M5076 sarcoma in murine, producing maximum increased life spans of 75% [7].
References:
[1] Zhang T.Y., et al. Positive effects of treatment of donor cells with aphidicolin on the preimplantation development of somatic cell nuclear transfer embryos in Chinese Bama mini-pig (Sus Scrofa) Anim. Sci. J. 2012;83:103–110.
[2] Navarro-Serna S, et al. Effect of Aphidicolin, a Reversible Inhibitor of Eukaryotic Nuclear DNA Replication, on the Production of Genetically Modified Porcine Embryos by CRISPR/Cas9. Int J Mol Sci. 2022 Feb 15;23(4):2135.
[3] Odongo GA, et al. Optimization of the alkaline comet assay for easy repair capacity quantification of oxidative DNA damage in PBMC from human volunteers using aphidicolin block. DNA Repair (Amst). 2019 May;77:58-64.
[4] Park JH, et al. Nuclear localization of endothelial nitric oxide synthase and nitric oxide production attenuates aphidicolin-induced endothelial cell death. Nitric Oxide. 2021 May 1;109-110:12-19.
[5] Cinatl J, et al. Aphidicolin selectively kills neuroblastoma cells in vitro. Cancer Lett. 1992 Dec 24;67(2-3):199-206.
[6] Michaelis M, et al. Increased systemic efficacy of aphidicolin encapsulated in liposomes. Oncol Rep. 2005 Jan;13(1):157-60.
[7] O'Dwyer PJ, et al. Antitumor activity and biochemical effects of aphidicolin glycinate (NSC 303812) alone and in combination with cisplatin in vivo. Cancer Res. 1994 Feb 1;54(3):724-9.
| Cell experiment [1]: | |
|
Cell lines |
HeLa cells |
|
Preparation Method |
HeLa cells were synchronized by 24 h incubation with aphidicolin. After aphidicolin removal, cells were collected at different time stamps (0, 1.5, 4, 8, 12 and 24 h). DNA content was measured by flow cytometry by tracing the fluorescence intensity of cells. |
|
Reaction Conditions |
1 mg/ml; 0, 1.5, 4, 8, 12 and 24 h |
|
Applications |
Aphidicolin efficiently synchronizes HeLa cells. Late S/G2 phase was reached around 12 hours after aphidicolin removal. After 24 hours cells return to their original, unsynchronized distribution. |
| Animal experiment [2]: | |
|
Animal models |
2-week-old WT and DKO (E2F1/E2F2 double-knockout) mice |
|
Preparation Method |
In vivo BrdU labeling and γ-H2AX accumulation in pancreases derived from 2-week-old WT and DKO mice, after i.p. injection of vehicle (saline) or aphidicolin. |
|
Dosage form |
10 µg/g; i.p. |
|
Applications |
Treatment with aphidicolin (10 µg/g) completely abolishes the incorporation of BrdU and reduces the number of cells with pan-nuclear γ-H2AX staining in DKO cells. |
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References: Szczepański K, et al. Stability of cytoplasmic nanoviscosity during cell cycle of HeLa cells synchronized with Aphidicolin. Sci Rep. 2019 Nov 11;9(1):16486. | |
| Cas No. | 38966-21-1 | SDF | |
| Sinónimos | ICI 69653, NSC 234714 | ||
| Chemical Name | (3R,4R,4aR,6aS,8R,9R,11aS,11bS)-4,9-bis(hydroxymethyl)-4,11b-dimethyltetradecahydro-8,11a-methanocyclohepta[a]naphthalene-3,9-diol | ||
| Canonical SMILES | O[C@@]1(CC[C@@]23[C@@]([H])(CC[C@]4([C@@](C)([C@@H](CC[C@@]43C)O)CO)[H])C[C@@H]1C2)CO | ||
| Formula | C20H34O4 | M.Wt | 338.48 |
| Solubility | 50mg/mL in DMSO, 10mg/mL in methanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9544 mL | 14.7719 mL | 29.5438 mL |
| 5 mM | 0.5909 mL | 2.9544 mL | 5.9088 mL |
| 10 mM | 0.2954 mL | 1.4772 mL | 2.9544 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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